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Assay Detail

CHEMBL880573

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of [3H]-AVP binding to human V2 receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vasopressin V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.
Venkatesan AM, Grosu GT, Failli AA, Chan PS, Coupet J, Saunders T, Mazandarani H, Ru X.
Bioorg Med Chem Lett (2005) 15 : 5003 -5006
PubMed 16153837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.51 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49429 LIXIVAPTAN 3.0 1 9.00
CHEMBL196737 1 7.24
CHEMBL380579 1 7.02
CHEMBL424663 1 6.52
CHEMBL381248 1 6.41
CHEMBL197616 1 6.29
CHEMBL198931 1 5.70
CHEMBL372766 1 5.60
CHEMBL371055 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49429 LIXIVAPTAN IC50 = 1.0 nM 9.00
CHEMBL196737 IC50 = 58.0 nM 7.24
CHEMBL380579 IC50 = 96.0 nM 7.02
CHEMBL424663 IC50 = 300.0 nM 6.52
CHEMBL381248 IC50 = 390.0 nM 6.41
CHEMBL197616 IC50 = 510.0 nM 6.29
CHEMBL198931 IC50 = 2000.0 nM 5.70
CHEMBL372766 IC50 = 2500.0 nM 5.60
CHEMBL371055 IC50 = 15000.0 nM 4.82